Colon Targeting of Naringin for Cytoprotection against Ulcerative Colitis: In Vitro-In Vivo Study

Borg, Thanaa Mohamed; Mohamed, Elham Abdelmonem; Naggar, Eman Ebrahim El; Elsheakh, Ahmad R.

doi:10.9790/3008-1202012329

Cited by 1 publication

(1 citation statement)

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“…Therefore, colon-targeted tablets of this drug based on coats of EUD L100-55 combined with hydroxypropyl methylcellulose were successfully prepared and evaluated in our laboratory. 26 In addition, our previous study indicated that naringin colon targeting was attained due to the drug release retardation that was related to the swelling rates of the coats that depended on the release retardant concentration. Thus, it was worth to prepare directly compressed coated tablets for colonic delivery of the naturally occurring naringin employing mixtures of pH-sensitive EUD-L and time-dependent polymers other than hydroxypropyl methylcellulose including EC, ALG and SCMC as compression coating.…”

Section: Introductionmentioning

confidence: 99%

<p>Colon Targeting of Naringin for Enhanced Cytoprotection Against Indomethacin-Induced Colitis in Rabbits</p>

Naggar¹,

Mohamed²,

Borg³

et al. 2020

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Background: Naringin is a promising anti-inflammatory drug against various disorders including ulcerative colitis. However, its oral bioavailability is low (8%) possibly due to cleavage at the upper gut. Consequently, colon targeting would be necessary for drug protection at the upper gut, enhanced oral bioavailability and potentiated cytoprotection against colitis. Methodology: This study involved the formulation of compression-coated tablets of naringin employing mixtures of pH-sensitive Eudragit L100-55 (EUD-L100-55) and different time-dependent polymers including ethyl cellulose (EC), sodium alginate (ALG) and sodium carboxymethyl cellulose (SCMC). Drug-polymer interaction during release was assessed using Fourier transform-infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Tablets were evaluated in vitro. Surface morphology of the optimized tablets either before or after exposure to the different release media was examined employing scanning electron microscopy (SEM). Cytoprotection potential of the optimized tablets against indomethacin-induced colitis in rabbits was screened and compared to core tablets through a histopathological examination of colon, measurement of serum perinuclear antineutrophil cytoplasmic antibodies (pANCA) and immunohistochemical localization of tumor necrosis factor-alpha (TNF-α). Results: FT-IR and DSC results may indicate drug-polymers interaction during release. Release retardation could be related to polymer swelling that was in the order of SCMC > ALG > EC. SEM examination indicated more porous coats at the buffers relative to the acidic medium. Colon targeting was expected in case of coats of 5% ALG, 5% SCMC and 10% EC (w/w) in combination with EUD-L100-55; thus, they were selected for in vivo evaluation. Effective cytoprotection of selected tablets against indomethacin-induced colitis was indicated by a significant (P<0.05) reduction in mucosal damage, serum levels of pANCA and TNF-α expression compared to untreated colitis and core-pretreated groups. Compared to EC, higher cytoprotection potential of ALG-and SCMC-based tablets was reflected by lower concentration (5% w/w) to provide cytoprotection against indomethacin-induced colitis.

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Section: Introductionmentioning

confidence: 99%